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APETx2

Catalog N: 07APE002

apetx2
 
 
 

 

Apetx2: Toxin properties

APETx2 is a toxin that was originally isolated from Anthopleura elegantissima (Sea anemone). APETx2 selectively blocks the H(+)-gated sodium channel ASIC3 (ACCN3). The blockage is rapid and reversible. This toxin does not block isoform ASIC1a and isoform ASIC1b of ASIC1 (ACCN2), nor ASIC2 (ACCN1). It also inhibits the heteromeric ASIC2b-ASIC3 channel, and has less affinity for ASIC1b-ASIC3, ASIC1a-ASIC3, and no effect on the ASIC2a-ASIC3 channels. IC50 is 63 nM on ASIC3 channel. IC50 is 117 nM on ASIC2b-ASIC3 heteromeric channel. IC50 is 0.9 µM on ASIC1b-ASIC3 heteromeric channel. IC50 is 2 µM on ASIC1a-ASIC3 heteromeric channel.

Product Specification

AA sequence: H-Gly-Thr-Ala-Cys4-Ser-Cys6-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys20-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys30-Arg-Tyr-Phe-Leu-Gly-Thr-Cys37-Cys38-Thr-Pro-Ala-Asp-OH
(Disulfide bonds between Cys4-Cys37, Cys6-Cys30 and Cys20-Cys38)
Length (aa): 42
Formula: C196H280N54O61S6
Molecular Weight: 4561.13 Da
Appearance: White lyophilized solid
Solubility: water and saline buffer
CAS number: not available
Source: Synthetic
Purity rate: > 95%

Price & Quantities

  • 100 µg : 200 €
  • 500 µg : 500 €
  • 1 mg : 850 €

Other quantities available upon request

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References

  • Blanchard MG, Rash LD, Kellenberger S. (2011) Inhibition of voltage-gated Na(+) currents in sensory neurons by the sea anemone toxin APETx2. Br J Pharmacol. 2011 Sep 22. doi: 10.1111/j.1476-5381.2011.01674. PubMed link
  • Tsuchimochi H, Yamauchi K, McCord JL, Kaufman MP. (2011) Blockade of Acid Sensing Ion Channels Attenuates the Augmented Exercise Pressor Reflex in Rats with Chronic Femoral Artery Occlusion.J Physiol. 2011 Oct 17. PubMed link
  • Chagot, B., Escoubas, P., Diochot, S., Bernard, C., Lazdunski, M., and Darbon, H. (2005) Solution structure of APETx2, a specific peptide inhibitor of ASIC3 proton-gated channels, Protein Sci 14, 2003-2010. PubMed link
  • Diochot, S., Baron, A., Rash, L. D., Deval, E., Escoubas, P., Scarzello, S., Salinas, M., and Lazdunski, M. (2004) A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons, EMBO J 23, 1516-1525. PubMed link

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